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Assay Detail

CHEMBL5228260

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]flunitrazepam from CBR receptor in rat brain cortex membrane incubated for 20 mins by liquid scintillation spectrometer method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Exploring Translocator Protein (TSPO) Medicinal Chemistry: An Approach for Targeting Radionuclides and Boron Atoms to Mitochondria.
Giordani A, Menziani MC, Moresco RM, Matarrese M, Paolino M, Saletti M, Giuliani G, Anzini M, Cappelli A.
J Med Chem (2021) 64 : 9649 -9676
PubMed 34254805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.77 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54349 ALPIDEM 4.0 1 9.00
CHEMBL12 DIAZEPAM 4.0 1 8.25
CHEMBL338738 1 6.07
CHEMBL134590 1 -
CHEMBL334887 1 -
CHEMBL5283306 1 -
CHEMBL335049 1 -
CHEMBL136030 1 -
CHEMBL137730 1 -
CHEMBL135408 1 -
CHEMBL335923 1 -
CHEMBL97269 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54349 ALPIDEM IC50 = 1.0 nM 9.00
CHEMBL12 DIAZEPAM IC50 = 5.6 nM 8.25
CHEMBL338738 IC50 = 860.0 nM 6.07
CHEMBL134590 IC50 > 1000.0 nM -
CHEMBL334887 IC50 > 1000.0 nM -
CHEMBL5283306 IC50 > 1000.0 nM -
CHEMBL335049 IC50 > 1000.0 nM -
CHEMBL136030 IC50 > 1000.0 nM -
CHEMBL137730 IC50 > 1000.0 nM -
CHEMBL135408 IC50 > 1000.0 nM -
CHEMBL335923 IC50 > 1000.0 nM -
CHEMBL97269 IC50 > 1000.0 nM -